Abstract: Disclosed are methods for treatments of conditions involving CD47 upregulation using a compound of formula (I): Variables R1-R9, X, and Het are defined therein. Also disclosed are methods for increasing phagocytosis of a cell using such a compound and pharmaceutical compositions each containing the compound and an anti-cancer agent.

Abstract: Benzimidazole compounds of formula (I), shown below, are disclosed. The compounds are potent human glutaminyl cyclase inhibitors. Also disclosed is a pharmaceutical composition containing one of these compounds and a pharmaceutical acceptable carrier, as well as a method of treating Alzheimer's disease or Huntington's disease by administering to a subject in need thereof an effective amount of such a compound.

Abstract: Benzimidazole compounds of formula (I), shown below, are disclosed. The compounds are potent human glutaminyl cyclase inhibitors. Also disclosed is a pharmaceutical composition containing one of these compounds and a pharmaceutical acceptable carrier, as well as a method of treating Alzheimer's disease or Huntington's disease by administering to a subject in need thereof an effective amount of such a compound.

Abstract: Disclosed herein is an expression system and uses thereof. The expression system comprises two vectors that express two fusion proteins and a glutaminyl cyclase (QC) with E45Q mutation, so as to autonomously produce a target protein having a N-terminal pyroglutamate (pGlu) residue in a host cell. The first fusion protein is composed of a maltose binding protein (MBP) and a tobacco etch virus protease (TEVP); and the second fusion protein includes in sequence, a thioredoxin, a S-tag, a linker having a TEVP recognition site therein, a target protein, and a (His)-6-tag. The second fusion protein is cleaved by the TEVP that is expressed by the first fusion protein, and then catalyzed by QC with E45Q mutation so as to autonomously produce the target protein having a N-terminal pGlu residue in the host cell.

Abstract: Disclosed herein is an expression system and uses thereof. The expression system comprises two vectors that express two fusion proteins and a glutaminyl cyclase (QC) with E45Q mutation, so as to autonomously produce a target protein having a N-terminal pyroglutamate (pGlu) residue in a host cell. The first fusion protein is composed of a maltose binding protein (MBP) and a tobacco etch virus protease (TEVP); and the second fusion protein includes in sequence, a thioredoxin, a S-tag, a linker having a TEVP recognition site therein, a target protein, and a (His)-6-tag. The second fusion protein is cleaved by the TEVP that is expressed by the first fusion protein, and then catalyzed by QC with E45Q mutation so as to autonomously produce the target protein having a N-terminal pGlu residue in the host cell.

Abstract: A crystalline structure of glutaminyl cyclase (QC) is described. Also described are the methods of preparing the crystalline structure of QC and the methods for identifying candidate inhibitors of QC. In addition, a structural basis for the rational design or identification of new inhibitors that may be used to treat QC-associated disorders is also described.

Abstract: A vector for expressing a soluble glutaminyl cyclase (QC) in bacterial cells is described. The vector contains a sequence encoding a fusion QC, which has a fusion protein tag selected from a Nus protein tag or a thioredoxin (Trx) tag, a QC, and a linker having at least one (His)x-tag between the QC and the fusion protein tag, in which x is an integer of at least 6. Methods for expressing a soluble glutaminyl cyclase (QC) by the vector are also described.

Abstract: A crystalline structure of glutaminyl cyclase (QC) is described. Also described are the methods of preparing the crystalline structure of QC and the methods for identifying candidate inhibitors of QC. In addition, a structural basis for the rational design or identification of new inhibitors that may be used to treat QC-associated disorders is also described.

Abstract: A crystalline structure of glutaminyl cyclase (QC). is described. Also described are the methods of preparing the crystalline structure of QC and the methods for identifying candidate inhibitors of QC. In addition, a structural basis for the rational design or identification of new inhibitors that may be used to treat QC-associated disorders is also described.

Abstract: The present invention relates to a vector for expressing a soluble glutaminyl cyclase (QC) containing a sequence encoding QC, a fusion protein tag upstream of the sequence encoding QC, and a linker having at least one (His)x-tag between the sequence encoding QC and the fusion protein tag, wherein x is an integer of at least 6. Methods for expressing a soluble glutaminyl cyclase (QC) by the vector of the present invention are also provided.

Abstract: The invention relates to a crystalline structure of glutaminyl cyclase (QC). The invention also relates to the methods of preparing the crystalline structure of QC and the methods for identifying candidate inhibitors of QC. This invention further provides a structural basis for the rational design or identification of new inhibitors that may be used to treat QC-associated disorders.